Studies on the Mechanism of Action of the Gastric H+,K+-ATPase Inhibitor SPI-447.

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  • Tsukimi Yasuhiro
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Ushiro Toshihisa
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Yamazaki Takashi
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Ishikawa Harumi
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Hirase Jyoji
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Narita Mitsuhiro
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Nishigaito Toshiki
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Banno Kimiko
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Ichihara Toshio
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan
  • Tanaka Hironori
    Department of New Drug Research Laboratories,Technical Headquarters,Shinnippon Pharmaceutical,Inc.,370 Mita,Kishiwada 596-0808,Japan

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抄録

3−Amino−5−methyl−2(2−methyl−3−thienyl)−imidazo[1, 2−a]thieno[3, 2−c]pyridine, SPI−447, is a potent gastric H+, K+−ATPase inhibitor, but a detailed mechanism of the inhibition is unknown.This study was designed to investigate the mechanism by which SPI−447 inhibits gastric H+, K+−ATPase.For this purpose, the inhibitory action of SPI−447 on gastric H+, K+−ATPase from porcine gastric mucosa was compared with that of omeprazole(an irreversible inhibitor)and SCH28080(a reversible inhibitor).All compounds produced dose−dependent inhibition of gastric H+, K+−ATPase, and the inhibitory intensities were increased under acidic conditions.The anti−H+, K+−ATPase actions of SPI−447 and SCH28080 were attenuated by dilution, but not influenced by glutathione pretreatment.In contrast, that of omeprazole was not influenced by dilution, but was suppressed by glutathione pretreatment.KCl addition reversed the inhibition of H+, K+−ATPase−mediated H+−transport by SPI−447 and SCH28080, but had no effect on that by omeprazole.The anti−gastric H+, K+−ATPase action of SPI−447 was additive with that of SCH28080.SPI−447 and SCH28080 had no effect on Na+, K+−ATPase activity.These findings indicated that the inhibitory mechanism of SPI−447 on gastric H+, K+−ATPase was similar to that of SCH28080, but different from that of omeprazole;i.e., 1)reversible, 2)SH−group independent, 3)K+−competitive, and 4)highly specific against gastric H+, K+−ATPase.

収録刊行物

  • Jpn.J.Pharmacol.

    Jpn.J.Pharmacol. 82 (1), 21-28, 2000

    公益社団法人 日本薬理学会

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